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检索条件"任意字段=2012年中国药物制剂大会——中国药学会药剂专业委员会年会、亚洲阿登制药技术研讨会暨国际控释协会中国分会年会"

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Influence of hydrophilic solid lipid nanoparticles on the absorption of drug in gastrointestinal tract

Influence of hydrophilic solid lipid nanoparticles on the ab...

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2012年中国药物制剂大会——中国药学会药剂专业委员会年会、亚洲阿登制药技术研讨会暨国际控释协会中国分会年会

作者： Hong Yuan,Chun-Yan Chen,Yong-Zhong Du,Fu-Qiang Hu College of Pharmaceutical Science,Zhejiang Uniersity,866 Yuhangtang Road.Hangzhou 310058,P.R.China,

Objective:During the last decade years,Caco-2 cell monolayers have been used as an intestinal model to evaluate the effect of delivery systems on drug permeation via transcellular and paracellular *** it lacks goblet,mucus-secreting and M-cells. In order to better simulate the endosomatic environment in vitro,HT-29 subclones have been used in co-culture with Caco-2 cells to mimic the small intestinal epithelial *** aim of this study was to evaluate the transport properties of solid lipid nanoparticles (SLN)across Caco-2 and mucus-secreting Caco-2/HT29 co-culture cell monolayers. Methods and Results:The SLN was prepared by aqueous solvent diffusion method in an aqueous *** was used as a lipid material,subsequently modified with polyethylene glycol(PEG)as modifying ***-fluorescein isothiocyanate(ODA-FITC)and doxorubicin(DOX)was used as a fluorescence marker and a model drug,*** permeation through Caco-2 cell monolayer was enhanced 3.1-fold,facilitated by the nanoparticles compared with Dox alone. Meanwhile,transport of PEG-modified SLN(pSLN)across Caco-2 and mucus-secreting Caco-2/HT29 co-culture cell monolayers was also ***,the stability of the nanoparticles in simulated gastrointestinal fluids was considerably increased by the PEG modifying around the particles as outermost coat to against *** the other hand,the permeation ability of pSLN decreased through Caco-2 cell monolayer while increased through a mucus-secreting Caco-2/HT29 co-culture,and also increased through excised intestinal mucosa of male Sprague-Dawley *** addition to increasing permeation ability,pSLN exhibited prolonged retention in the rat gut,which increase in the area under the curve(AUC)for DOX as compared to the PEG-free SLN. Conclusion:It is clear that nanoparticle surface properties are very important for intestinal *** this reason,nanoparticle surface characteristics can be tailored to optimiz

关键词： Caco-2 cells HT-29 cells solid lipid nanoparticles otcadecylamine-fluorescein isothiocyanate doxorubicin(DOX) solvent diffusion method Oral drug delivery

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Core-shell liponanoparticles for intraocular drug delivery to RPE

Core-shell liponanoparticles for intraocular drug delivery t...

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2012年中国药物制剂大会——中国药学会药剂专业委员会年会、亚洲阿登制药技术研讨会暨国际控释协会中国分会年会

作者： Li Gan~1,Jing Wang~(1,2),Jianping Liu~2,Yong Gan~(1,*) 1 Shanghai Institute of Materia Medica,Chinese Academy of Sciences,501 Haike Road,Shanghai 201203,China. 2 School of Pharmacy,China Pharmaceutical University,24 Tongjiaxiang,Nanjing 210009,China

Objectives:Most of the sight-threatening eye conditions,such as uveitis,age-related macular degeneration,and diabetic retinopathy are related to ***,retinal drug delivery is a challenging *** obstacles,such as short intraocular retention time and non-targeted biodistribution to the retina,have not been *** on these considerations,we are trying to formulate novel Hyaluronan-modified core-shell liponanoparticles(HA-LCS-NPs)to achieve efficient intravitreal drug delivery. Methods:Core-shell liponanoparticles(LCS-NPs)were prepared by hydrating a dried lipid film with chitosan nanoparticles (CS-NPs)***-LCS-NPs were obtained by covalent linkage of the glucuronic acid moiety of the targeting ligand HA to the primary amine of DOPE of the preformed liposomes *** uptakes of various nanosystems were evaluated on ARPE-19 *** vivo vitreous and retinal distributions of nanosystems were finally investigated. Results:The particle size of HA-LCS-NPs was about 450 nm,with zeta potential being about-20 *** uptake study with ARPE-19 cells showed that HA-LCS-NPs with higher HA density exhibited about 1.6-fold higher uptake than that with low HA *** HA molecular weight(200-400 kDa)resulted in improved intracellular uptake(of about 1.5-fold increase).After pretreating the ARPE-19 cells with a saturable amount of free HA(200-400 kDa),the HA-LCS-NPs uptake was significantly reduced. As shown in CLSM images,most HA-LCS-NPs overcame the vitreous barriers and passed through the inner limiting membrane. More red fluorescence was appeared at the retinal pigment epithelium layer than CS-NPs group. Conclusions:HA-LCS-NPs with improved intracellular uptake and superior penetrating ability across the vitreous and retinal barriers to RPE might present as a promising efficient retinal drug delivery system.

关键词： Hyaluronan chitosan Liponanoparticles RPE Intravitreal movement

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Study on the Preparation and Characteristics of Artemisinin-Loaded Solid Lipid Nanoparticle(ART-SLN) Formulation

Study on the Preparation and Characteristics of Artemisinin-...

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2012年中国药物制剂大会——中国药学会药剂专业委员会年会、亚洲阿登制药技术研讨会暨国际控释协会中国分会年会

作者： Fu Chuan~1,Yu Ji-ying~2,Zou Jing~2,He Lin~2,Huang Yuan~1 1.West China School of Pharmacy,Sichuan University,Chengdu,610041,China 2.Department of Pharmacy,Sichuan Academy of Medical Sciences & Sichuan Provincial People's Hospital,Chengdu,610072,China

Objective:Solid lipid nanoparticle（SLN）with artemisinin was developed for pulmonary administration because of its poor water *** formula and preparation of artemisinin-loaded solid lipid nanoparticle（ART-SLN）were optimized and its characteristics of ART-SLN were also studied. Method:Trilaurine was chosen as the solid matrix,soybean lecithin and pluronic F68 as the surfactant and ART-SLN was prepared by solvent emulsification evaporation *** encapsulation efficiency（EE）and drug loading（DL）of the ART-SLN were determined by salting-out *** method with a pre-column derivation was selected to determine the content of *** linear range of ART is ***-mL"*** accuracy of the method and the precision intra-day and inter-day were 100.97%±2.46%,0.82%±0.61%and 4.88%±1.17%*** results of methodology showed that this method was suitable for the determination of the EE and DL of *** preparation technology was first studied with single-factor *** ultrasonic power and time,types of organic solvents,the ration of organic phase to water,the amount of ART,soybean lecithin and trilaurine and the concentration of F68 were selected as the *** best results were obtained while the ultrasonic power was 200w and the ultrasonic time was 45s and the volume ratio was 1:*** the EE is more than 90%in all experiments,it was not selected as the evaluation index of *** of that,the particle size and drug loading were selected as the index to evaluate in the subsequently *** composite design-response surface methodology（CCD）has been used to further optimize the formulation and *** factors including the dosage（Xl）,the amount of soybean phosphilipids（X2）and the concentration of F68（X3）were selected to design the *** results were fitted with multivariate quadratic equation by Metlab Software and the binomial equations were as follows: SIZE=157.86+1.47X1+405.09X2-212.32X3+0.01X

关键词： artemisinin solid lipid nanoparticle(SLN) Central composite design-response surface methodology(CCD)

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Studies on lactoferrin nanoparticles of gambogic acid for oral delivery

Studies on lactoferrin nanoparticles of gambogic acid for or...

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2012年中国药物制剂大会——中国药学会药剂专业委员会年会、亚洲阿登制药技术研讨会暨国际控释协会中国分会年会

作者： Xiao-Pan Wang~1,Zhen-Hai Zhang~(1,2),Waddad YAyman~1,Hui-Xia Lv~1,Jian-PingZhou~1. 1 Department of Pharmaceutics,China Pharmaceutical University,Nanjing,China,210009. 2 Jiangsu Province Academy of Traditional Chinese Medicine,Nanjing,China,210028.

Aim:Lactoferrin(Lf),a mammalian cationic iron-binding glycoprotein belonging to the transferrin(Tf)family,has been widely used in a number of areas from infant diarrhea and support for newborn growth to food and pharmaceutical *** this study,lactoferrin nanoparticles were used as carrier of gambogic acid(GA)to increased its solubility,oral absorption time and hence reduce its side ***:gambogic acid lactoferrin nanoparticles(GL-NPs)were prepared by using Nanoparticle Albumin-Bound *** the physical and chemical properties of GL-NPs including particle size,zeta potential,drug loading capacity,entrapment efficiency were *** to explore the intestinal absorption mechanism of GL-NPs,in situ intestinal perfusion experiment was *** in vivo and in vitro anti-tumor activity of GL-NPs were investigated and compared with Arginine solution of ***:GL-NPs successfully loaded GA with encapsulation efficiency of 92.3±7.2% and drug loading of 9.04±0.7%.The mean size of GL-NPs was about 150nm withζpotential of+20 *** results showed that GA dispersed inside Lf-NPs as an amorphous form or molecular *** results of in situ intestinal perfusion showed that GL-NPs was transformed from passive diffusion into active transport or facilitated diffusion,and suggested Lf receptor might play a role in the transcytosis of *** assay of GL-NPs showed almost an equal effect with Arginine solution of GA(Arg-GA)as in inhibition against HepG2 cell lines with *** inhibitory rate against S180 tumor in mice after oral administration of GL-NPs was up to 86.01%which wasl.39 folds of intravenous injection of *** result indicated that oral administration of GL-NPs could increase the anti-tumor activity of GA to a large extent,while avoiding the toxicity induced by ***:In conclusion,the results of present research exhibited lactoferrin as a potential vehicle to enhance oral absorption of hydr

关键词： gambogic acid lactoferrin nanparticles oral administration

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Active tumor-targeted drug delivery system:doxorubicin-hy d-PEG-folate conj ugate

Active tumor-targeted drug delivery system:doxorubicin-hy d-...

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2012年中国药物制剂大会——中国药学会药剂专业委员会年会、亚洲阿登制药技术研讨会暨国际控释协会中国分会年会

作者： Wei-liang Ye,Si-yuan Zhou~* Department of Pharmaceutics,School of Pharmacy,Fourth Military Medical University,17~# Changle West Road,Xi 'an,710032.

Aim:Doxorubicin(DOX)is a highly potent chemotherapeutic agent that is widely used to treat various types of cancers,including breast and urothelial ***,its severe side effects,such as cardiotoxicity,remain as a major *** overcome these limits,more effective and active targeting system is needed to enhance intracellular uptake of drug in cancerous cells at the tumor ***:A PEG based folate mediated active tumor targeting delivery systems for DOX was designed and *** this system,DOX was conjugated with PEG by hydrazone bond(DOX-hyd-PEG-FA)or by amide bond(DOX-ami-PEG-FA).The drug loading of the conjugates was detected by HPLC method,and the drugs release characteristic was performed in different pH media in *** KB cells(folate receptor over-expression)and A549 cells(folate receptor low-expression)were selected to study the cytotoxicity of the conjugates,meanwhile the effect of exogenous folic acid on the cytotoxicity of the conjugates was also observed. The uptake of DOX and its conjugates by tumor cells were analyzed by flow cytometry and fluorescence *** intracellular distribution of conjugates was studied by using laser scanning confocal ***:The rate and amount of DOX release from the DOX-hyd-PEG-FA were strongly dependent on the pH of the ***-hyd-PEG-FA showed a much faster DOX release at pH 5.0 than at pH *** rate and amount of DOX release from the DOX-ami-PEG-FA was independent on the pH of the *** with DOX-hyd-PEG DOX-hyd-PEG-FA could increase the intracellular accumulation of DOX in short time and showed a DOX translocation from lysosomes to nucleus in KB ***-hyd-PEG-FA could deliver DOX to nucleus in KB cells in a time dependent *** cytotoxicity of DOX-hyd-PEG-FA on KB cells was much higher than that of DOX-ami-PEG-FA and DOX-hyd-PEG Meanwhile,the cytotoxicity of DOX-hyd-PEG-FA on KB cells was much higher than that on A549 *** cytotoxicity and intra

关键词： poly(ethylene glycol)(PEG) pH-sensitive tumor-targeted doxorubicin folate receptor cellular uptake cytotoxicity

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Docetaxel loaded Pluronic P105/F127 mixed micelles against Drug-Resistant Lung Adenocarcinoma Cell Line A549/Taxol:in vitro and in vivo evaluation

Docetaxel loaded Pluronic P105/F127 mixed micelles against D...

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2012年中国药物制剂大会——中国药学会药剂专业委员会年会、亚洲阿登制药技术研讨会暨国际控释协会中国分会年会

作者： Liangcen Chen~a,Xinyi Jiang~a,Xiaoling Fang~(a*) a Key Laboratory of Smart Drug Delivery(Fudan University),Ministry of Education & PLA,Department of Pharmaceutics,School of Pharmacy,Fudan University,Lane 826,Zhangheng Road,Shanghai 201203,China

The aim of this study was to investigate the antitumor effect of docetaxel(DTX)loaded Pluronic P105/F127 mixed micelles(PF-DTX)against drug-resistant Lung Adenocarcinoma Cell Line A549/*** loaded Pluronic P105/F127 mixed micelles was prepared by thin-film hydration method and optimized using central composite *** of multidrug resistance(MDR)by Pluronic mixed micelles was evaluated in Taxol-resistant Human lung adenocarcinoma cell line A549 (A549/Taxol).In vitro cytotoxicity was determined by CCK8 assay,while cellular apoptosis was detected by cell nuclei staining and Annexin V-FITC apoptosis detection *** cycle arrest was also confirmed by flow ***,in vivo antitumor efficacy of PF-DTX was extensively evaluated in comparison with *** in vitro release of DTX from the mixed micelles presented a sustained-release *** in vitro cytotoxicity assay showed that on the sensitive A549 cells,the IC50 values for Taxotere and PF-DTX were similar,while on A549/Taxol cells,IC50 values of PF-DTX(0.059ug/ml)was much lower than those of Taxotere injection(0.593μg/ml)and the free DTX(0.857μg/ml),which showed superior hypersensitizing effect on MDR *** enhanced anti-cancer efficacy of PF-DTX in vitro was associated with DTX-induced apoptosis and cell arrest in the G2/M *** BALB/c mice bearing A549/Taxol tumor xenografts,stronger antitumor efficacy was shown in PF-DTX group,with good correlation between in vitro and in ***,it was concluded that Docetaxel loaded Pluronic P105/F127 mixed micelles significantly enhanced the anti-cancer activity of DTX and might be considered a promising drug delivery system to overcome MDR in lung cancer.

关键词： Docetaxel Pluronic A549/Taxol Multidrug resistance micelles anticancer efficacy

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A thermosensitive siRNA delivery system for dendritic cells targeting

A thermosensitive siRNA delivery system for dendritic cells ...

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2012年中国药物制剂大会——中国药学会药剂专业委员会年会、亚洲阿登制药技术研讨会暨国际控释协会中国分会年会

作者： Lin ZHOU,Jie PU,Li ZHU,Qing-ri CAO,Jing-hao CUI College of Pharmaceutical Science,Soochow University,Suzhou,215123,China.

Purpose:Dendritic cells（DCs）,as professional antigen presenting cells（APC）,play an important role both in natural immunity and acquired *** their clinical applications were limited due to their short lifespan and small quantities in *** has been shown that the expression of Bak can promote the apoptosis of *** interference is a specific and efficient approach to cause some gene *** the research of siRNA delivery system targeting Bak will be expected to increase its antigen presenting,promote the immune response and enhance anti-tumor ***,based on the surface expression of DEC-205 receptor on DCs,the DEC-205 modified poloxamer-g-chitosan containing siRNA was synthesized to prepare thermo-sensitive micelles,and the nano-carriers were then characterized with respect to the pharmaceutical properties in order to provide the evidence of the optimizing carrier design and further in vivo evaluation. Method:DEC-205 modified poloxamer-g-chitosan micelles containing siRNA were prepared based on our previous *** physicochemical properties of polymer micelles（PMs）,such as size,Zeta potential,siRNA encapsulation efficiency and cytotoxicity were *** were generated and activated from murine bone marrow ***,the uptaken of PMs by DCs were observed by fluorescence microscope and flow *** of siRNA loaded PMs on the expression of Bak in DCs and viability of DCs were confirmed with Western blot and cell death detection kit,respectively. Result:The structure of poloxamer-g-chitosan was confirmed by IR,NMR and thermo gravimetric *** value of CMC and LCST were（1.39±0.08）×10-6 *** 40℃.The concentrations of PMs and siRNA were 0.5 *** 120 *** average size and Zeta potential of siRNA loaded PMs were（230±4.1）nm and +（13.98±0.8）mV,*** entrapment efficiency of siRNA was（80.2±2.93）%.Endocytosis rate of the PMs containing FAM-siRNA was higher than FAM-siRNA *** mod

关键词： dendritic cells siRNA thermo-sensitive polymer micelles,DEC-205

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Dual-Targeting Liposomal Doxorubicin for Therapy of Glioma

Dual-Targeting Liposomal Doxorubicin for Therapy of Glioma

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2012年中国药物制剂大会——中国药学会药剂专业委员会年会、亚洲阿登制药技术研讨会暨国际控释协会中国分会年会

作者： Xiaoli Wei,Zhixin Zhang,Xishan Chen,Changyou Zhan,Zhanmei Feng,Weiyue Lu~* Department of Pharmaceutics,School of Pharmacy,Fudan University. Key Laboratory of Smart Drug Delivery(Fudan University),Ministry of Education & PLA,China.826 Zhangheng Road,Shanghai 201203,China.

Objective:Glioma is one of the most common types of brain *** extensive efforts have been made to improve efficacy of chemotherapy,there is no effective treatment currently *** order to treat glioma thoroughly and safely,liposomes modified with both a brain-targeted moiety,d-CDX,and a glioma-targeted moiety,c（RGDyK）,were developed for transporting doxorubicin across the blood-brain barrier and then targeting brain glioma,which were expected to realize "dual-targeting drug delivery". Methods & Results:Previously a 16 residue peptide L configuration CDX was reported by us to facilitate drug delivery systems to cross the blood-brain *** improve the in vivo stability of this peptide,here we synthesized D configuration CDX via solid phase peptide synthesis *** the present work,binding of the peptides to the neuronal nAChRs was assessed by measuring their ability to inhibit the binding of I-α-bungarotoxin to the *** was demonstrated that d-CDX have higher binding affinity with nAChRs and the ICvalues were 441.6nM（l-CDX）and 84.5nM（d-CDX）*** dual-targeting liposomes could be uptaken by both primary rat brain capillary endothelial cells and U87 cells in *** the near-infrared dye DIR qualitative biodistribution results in vivo and the 5-FAM fluorescent images of the U87 bearing nude brain slides demonstrated the preferable accumulation of such dual-targeting liposomes in the tumor *** median survival time of U87 bearing nudes after administering dual-targeting liposomal doxorubicin（37 days）was significantly longer than that for free doxorubicin（28 days）, liposomal doxorubicin（29.5 days）,RGD-liposome loading Dox（31Days）and d-CDX-liposome loading Dox（33 days）. Conclusion:This dual-targeting liposomes may provide a potential carrier to improve the therapeutic efficacy of doxorubicin on glioma.

关键词： dual-targeting liposome blood-brain barrier glioma doxorubicin

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Amphiphilic PELA microspheres of recombinant human growth hormone

Amphiphilic PELA microspheres of recombinant human growth ho...

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2012年中国药物制剂大会——中国药学会药剂专业委员会年会、亚洲阿登制药技术研讨会暨国际控释协会中国分会年会

作者： Yi Wei,Yu-Xia Wang,Guang-Hui Ma National Key Laboratory of Biochemical Engineering,Institute of Process Engineering,Chinese Academy of Sciences, Beijing,100190,PR China.

Objective:Recombinant Human growth hormone(rhGH)has been used for treatment of pediatric short stature caused by growth hormone deficiency,Turner's syndrome,and chronic renal *** to its short half-life,the current rhGH product requires frequent subcutaneous injection daily or three times a week,which leads to poor patient ***,development of a sustained-release rhGH formulation could ameliorate patient quality of life and alleviate the burden of expense attendant on frequent ***:The coarse double emulsions were further refined by extruding the emulsion through the SPG *** obtained uniform double emulsions were solidified to form ***:As shown in Fig.a-c,all microspheres possessed narrow size distributions around 6 urn,which contributed to good process reproducibility and repeatable drug release behavior. PELA-1 microspheres showed a total of 79.8%rhGH release within 66 days,whereas PELA-2 and PELA-3 microspheres released about 76.1%and 20.1%rhGH,respectively(Fig.d).The reason for the difference among the above release profiles was mainly due to the varied erosion rate of polymeric matrix by hydrolysis in *** decrease in molecular weight as well as high ratios of mPEG, water penetrability would be enhanced and consequently degradation rate of the polymer could be ***-1 microspheres released mostly the monomelic rhGH,while a large part of the rhGH released from PELA-2 and PELA-3 microspheres was aggregates and hydrolyzed fragments due to the acidic microenvironment(Fig.e).Since PELA-1 possessed the highest ratio of hydrophilic mPEG,which can be hydrated more easily in the releasing medium,its microspheres could swell more readily and the water-soluble acids produced by the polyester hydrolysis could diffuse out more ***:These results suggest that the PELA hydrophilicity played an important role on protein incomplete release and stability,thus offering an alternative to adjust

关键词： PELA microspheres sustained release rhGH

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Preparation and Characterization of Silk Fibroin-Liposomes for Ophthalmic Drug Delivery

Preparation and Characterization of Silk Fibroin-Liposomes f...

引用

2012年中国药物制剂大会——中国药学会药剂专业委员会年会、亚洲阿登制药技术研讨会暨国际控释协会中国分会年会

作者： Y.X.Dong,P.Dong,D.Huang,X.Pan,C.B.Wu Pharmaceutics School of Pharmaceutical Sciences Sun Yat-Sen University,University Town,Guangzhou 510006,China

OBJECTIVE To prepare and characterize silk fibroin（SF）-liposomes and study the application in the ocular drug delivery systems. METHODS The extracted silk fibroin was dissolved in CaCl-EtOH-HO solution for 2h,4h,6h,8h at 78℃.The molecular weight, secondary structure,stability and concentrations of SF were determined using SDS-PAGE,FTIR,CD and *** assay was performed to assess survival rates of human corneal epithelial cells（HCEC）after exposure to 0.25,0.5,1.0 or 2.0%（w/v）SF solution （n=5）after 24h and 48h recovery *** loaded liposomes were prepared by the ethanol injection method,then SF was coated on the liposomes and insolubilized with *** morphology,entrapment efficiency,in vitro release and permeability through the isolated cornea of SF-liposomes were *** red and FITC were labeled to liposomes and SF,respectively. HCEC were cultured to study the cellular uptake of SF and SF-liposomes by confocal laser scanning microscopy. RESULTS The molecular weight of SF peptide chains were decreased as the degradation time ***,the secondary structure of SF remained in silk I regardless of the degradation *** SF was stable for at least 18 months when stored at room temperature.A simple UV method for determination of SF was *** calibration curve was linear in the range of（0.1～1.0） mg/ml with correlation coefficient of *** survival values,as determined by microplate reader,were above 80%after 24 hours of exposure to SF *** significant differences were observed among the different SF ***,the survival rate of HCEC became higher after 48h ***'s more,there existed a positive correlation between cell survival rates and SF *** highest survival value,which was over 200%,was observed at a 2.0%concentration of SF. Ibuprofen liposomes prepared by aqueous SF had a relative narrow size distribution ranging from 200 nm to 300 *** encapsulation efficiency of i

关键词： silk fibroin liposomes sustained release cellular uptake cytotoxicity

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